EP3434677A4 - Polymorph of dppiv inhibitor maleate and preparation method therefor - Google Patents

Polymorph of dppiv inhibitor maleate and preparation method therefor Download PDF

Info

Publication number: EP3434677A4
Authority: EP; European Patent Office
Prior art keywords: polymorph; preparation; method therefor; dppiv inhibitor; maleate
Prior art date: 2016-03-22
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Granted

Application number

EP17769393.4A

Other languages

German (de)

French (fr)

Other versions

EP3434677A1 (en

EP3434677B1 (en

Inventor

Hong Liu

Jiang Wang

Jian Li

Jia Li

Jingya Li

Hualiang Jiang

Xiaomin Luo

Kaixian Chen

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Shanghai Institute of Materia Medica of CAS

Original Assignee

Shanghai Institute of Materia Medica of CAS

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2016-03-22

Filing date

2017-03-20

Publication date

2019-11-27

2017-03-20 Application filed by Shanghai Institute of Materia Medica of CAS filed Critical Shanghai Institute of Materia Medica of CAS

2019-01-30 Publication of EP3434677A1 publication Critical patent/EP3434677A1/en

2019-11-27 Publication of EP3434677A4 publication Critical patent/EP3434677A4/en

2023-05-03 Application granted granted Critical

2023-05-03 Publication of EP3434677B1 publication Critical patent/EP3434677B1/en

Status Active legal-status Critical Current

2037-03-20 Anticipated expiration legal-status Critical

Links

239000003112 inhibitor Substances 0.000 title 1
VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 title 1
238000002360 preparation method Methods 0.000 title 1
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 title 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Diabetes (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Endocrinology (AREA)
Emergency Medicine (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Hematology (AREA)
Obesity (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

EP17769393.4A 2016-03-22 2017-03-20 Polymorphs of dppiv inhibitor maleate and preparation method therefor Active EP3434677B1 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
CN201610165572.4A CN107216339B (en)	2016-03-22	2016-03-22	Polymorphism of DPPIV inhibitor maleate and preparation method thereof
PCT/CN2017/077278 WO2017162116A1 (en)	2016-03-22	2017-03-20	Polymorph of dppiv inhibitor maleate and preparation method therefor

Publications (3)

Publication Number	Publication Date
EP3434677A1 EP3434677A1 (en)	2019-01-30
EP3434677A4 true EP3434677A4 (en)	2019-11-27
EP3434677B1 EP3434677B1 (en)	2023-05-03

Family

ID=59899234

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
EP17769393.4A Active EP3434677B1 (en)	2016-03-22	2017-03-20	Polymorphs of dppiv inhibitor maleate and preparation method therefor

Country Status (8)

Country	Link
US (1)	US10640514B2 (en)
EP (1)	EP3434677B1 (en)
JP (1)	JP6921850B2 (en)
KR (1)	KR102160093B1 (en)
CN (1)	CN107216339B (en)
CA (1)	CA3018599C (en)
RU (1)	RU2732577C1 (en)
WO (1)	WO2017162116A1 (en)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP2786998A1 (en) *	2011-12-01	2014-10-08	Shanghai Institute of Materia Medica, Chinese Academy of Sciences	Thienyl [3, 2-d]pyrimidin-4-one compounds, preparation method, pharmaceutical compositions and use thereof

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IT1272290B (en) *	1994-06-20	1997-06-16	Avantgarde Spa	SALT OF L-CARNITINE AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN IT FOR THE TREATMENT OF SKIN DISEASES
JP4668536B2 (en) *	2001-12-20	2011-04-13	オーエスアイ・ファーマスーティカルズ・インコーポレーテッド	Pancreatic lipase inhibiting compounds, their synthesis and use
US8618115B2 (en) *	2005-10-26	2013-12-31	Bristol-Myers Squibb Company	Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them
BRPI0923121A2 (en) *	2008-12-23	2015-08-11	Boehringer Ingelheim Int	Saline forms of organic compounds
CN101817833B (en) *	2009-02-26	2013-03-06	中国科学院广州生物医药与健康研究院	DPP-IV inhibitor
WO2010125004A1 (en) *	2009-04-29	2010-11-04	Nerviano Medical Sciences S.R.L.	Cdk inhibitor salts
TW201204733A (en) *	2010-06-25	2012-02-01	Kowa Co	Novel condensed pyridine or condensed pyrimidine derivative, and medicinal agent comprising same
CN102311448B (en) *	2010-07-07	2014-02-19	中国科学院广州生物医药与健康研究院	Thieno-pyrimidone DPP-IV (dipeptidyl peptidase) inhibitor
CN102659813B (en) *	2012-05-23	2015-01-07	中国科学院上海药物研究所	2-((2-(3-aminopiperidine-1)-4-oxythiophene (3, 2-d) pyrimidine-3(4H)-methyl) polymorphic benzonitrile, and preparation method and pharmacological applications thereof
CN103709163B (en) *	2012-09-29	2016-12-21	齐鲁制药有限公司	Xanthine derivative, Preparation Method And The Use

2016
- 2016-03-22 CN CN201610165572.4A patent/CN107216339B/en active Active
2017
- 2017-03-20 WO PCT/CN2017/077278 patent/WO2017162116A1/en active Application Filing
- 2017-03-20 JP JP2018550390A patent/JP6921850B2/en active Active
- 2017-03-20 RU RU2018137076A patent/RU2732577C1/en active
- 2017-03-20 US US16/087,317 patent/US10640514B2/en active Active
- 2017-03-20 EP EP17769393.4A patent/EP3434677B1/en active Active
- 2017-03-20 CA CA3018599A patent/CA3018599C/en active Active
- 2017-03-20 KR KR1020187030145A patent/KR102160093B1/en active IP Right Grant

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP2786998A1 (en) *	2011-12-01	2014-10-08	Shanghai Institute of Materia Medica, Chinese Academy of Sciences	Thienyl [3, 2-d]pyrimidin-4-one compounds, preparation method, pharmaceutical compositions and use thereof

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
"Handbook of Pharmaceutical Salts - Properties, Selection, and Use", 1 January 2002, VERLAG HELVETICA CHIMICA ACTA; WILEY-VCH, Z?rich, Weinheim, article "Tables of Salt-Forming Acids and Bases", pages: 331 - 345, XP055247250 *
HILFIKER R ET AL: "Relevance of Solid-state Properties for Pharmaceutical products", 1 January 2006, 20060101, PAGE(S) 1 - 19, ISBN: 978-3-527-31146-0, XP002525043 *
MINO R CAIRA ED - MONTCHAMP JEAN-LUC: "Crystalline Polymorphism of Organic Compounds", TOPICS IN CURRENT CHEMISTRY; [TOPICS IN CURRENT CHEMISTRY], SPRINGER, BERLIN, DE, vol. 198, 1 January 1998 (1998-01-01), pages 163 - 208, XP008166276, ISSN: 0340-1022, [retrieved on 19990226], DOI: 10.1007/3-540-69178-2_5 *
RICHARD J BASTIN ET AL: "Salt Selection and Optimisation Procedures for Pharmaceutical New Chemical Entities", ORGANIC PROCESS RESEARCH AND DEVELOPMENT, AMERICAN CHEMICAL SOCIETY, US, vol. 4, no. 5, 19 July 2000 (2000-07-19), pages 427 - 435, XP008154792, ISSN: 1083-6160, [retrieved on 20000719], DOI: 10.1021/OP000018U *
See also references of WO2017162116A1 *

Also Published As

Publication number	Publication date
JP6921850B2 (en)	2021-08-18
CN107216339A (en)	2017-09-29
CN107216339B (en)	2021-05-04
US10640514B2 (en)	2020-05-05
EP3434677A1 (en)	2019-01-30
CA3018599A1 (en)	2017-09-28
WO2017162116A1 (en)	2017-09-28
KR102160093B1 (en)	2020-09-25
JP2019509325A (en)	2019-04-04
CA3018599C (en)	2021-04-20
EP3434677B1 (en)	2023-05-03
RU2732577C1 (en)	2020-09-21
KR20180120269A (en)	2018-11-05
US20190100529A1 (en)	2019-04-04

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